In Vitro Effects of the New Calcium Antagonist Lacidipine

Kawada, Toru; Sun, Hsiao-Tung; Nakazawa, Makoto; Imai, Shoichi

doi:10.1254/jjp.62.395

Cited by 12 publications

(6 citation statements)

References 38 publications

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“…Similar to other studies on itopride,7,16 we evaluated the AChE activity of itopride on the ileum and colon and found that neostigmine accelerated the propagation velocity of the ileum at lower concentrations and dose-dependently shortened the colonic transit time. This pattern was similar to those obtained with itopride, except at higher concentrations, in the ileum.…”

Section: Discussionsupporting

confidence: 70%

“…However there are a few in vitro studies to determine the stimulatory effect in the lower gut 15,16. Iwanaga et al16 compared itopride and physostigmine on contractile responses to ACh and carbachol and reported that itopride increased the amplitude of longitudinal muscle contractions and frequency of peristalsis in an isolated segment in guinea pig ileum.…”

Section: Discussionmentioning

confidence: 99%

“…Iwanaga et al16 compared itopride and physostigmine on contractile responses to ACh and carbachol and reported that itopride increased the amplitude of longitudinal muscle contractions and frequency of peristalsis in an isolated segment in guinea pig ileum. Because itopride enhanced only contractions induced by ACh and failed to increase spontaneous or stimulation-induced ACh release, they concluded that itopride stimulates ileal activity by prevention of ACh hydrolysis 16. In this study, the increase of the amplitude was demonstrated after administration of itopride with ACh, in concordance with previous studies on the increase of contractility.…”

Section: Discussionmentioning

confidence: 99%

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Effect of Itopride Hydrochloride on the Ileal and Colonic Motility in Guinea Pig In Vitro

et al. 2008

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PurposeItopride hydrochloride (itopride) inhibits acetylcholinesterase (AChE) and antagonizes dopamine D2 receptor, and has been used as a gastroprokinetic agent. However, its prokinetic effect on the small bowel or colon has not yet been thoroughly investigated. The aim of this study was to investigate the effects of itopride on motor functions of the ileum and colon in guinea pigs.Materials and MethodsThe distal ileum was excised and the activity of peristaltic contraction was determined by measuring the amplitude and propagation velocity of peristaltic contraction. The distal colon was removed and connected to the chamber containing Krebs-Henseleit solution (K-H solution). Artificial fecal matter was inserted into the oral side of the lumen, and moved toward the anal side by intraluminal perfusion via peristaltic pump. Colonic transit times were measured by the time required for the artificial feces to move a total length of 10 cm with 2-cm intervals.ResultsIn the ileum, itopride accelerated peristaltic velocity at higher dosage (10-10-10-6 M) whereas neostigmine accelerated it only with a lower dosage (10-10-10-9 M). Dopamine (10-8 M) decelerated the velocity that was recovered by itopride infusion. Itopride and neostigmine significantly shortened colonic transit at a higher dosage (10-10-10-6 M). Dopamine (10-8 M) delayed colonic transit time that was also recovered after infusion of itopride.ConclusionItopride has prokinetic effects on both the ileum and colon, which are regulated through inhibitory effects on AChE and antagonistic effects on dopamine D2 receptor.

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Section: Discussionsupporting

confidence: 70%

Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

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Effect of Itopride Hydrochloride on the Ileal and Colonic Motility in Guinea Pig In Vitro

et al. 2008

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“…In conscious dogs, itopride stimulates postprandial gastric motility and enhances gastric contraction evoked by ACh infusion (1). Itopride inhibits electric eel AChE (IC50=2.9 pM) (1) and enhances guinea pig ileum contraction evoked by ACh (2) in vitro. These results suggest that AChE inhibition is in volved in the mechanism of the itopride-induced stimula tion of gastric motility in conscious dogs.…”

Section: Discussionmentioning

confidence: 99%

Characterization of Acetylcholinesterase-Inhibition by Itopride

Iwanaga

Kimura

Miyashita

et al. 1994

Japanese Journal of Pharmacology

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ABSTRACT-Itopride is a gastroprokinetic benzamide derivative. This agent inhibited both electric eel acetylcholinesterase (AChE) and horse serum butyrylcholinesterase (BuChE). The IC50 of itopride with AChE (2.04±0.27 pM) was, however, 100-fold less than that with BuChE, whereas in the case of neostigmine with AChE (11.3±3.4 nM), it was 10-fold less. The recovery of AChE activity inhibited by 10-7 M neostigmine was partial, but that inhibited by upto 3 x 10-5 M itopride was complete when the reaction mix ture was subjected to ultrafiltration. Double reciprocal plots of the experimental data showed that both Km and Vmax were affected by itopride, suggesting that the inhibition is a "mixed" type, although primarily being an uncompetitive one. The inhibitory effect of itopride on cholinesterase (ChE) activity in guinea pig gastrointestine was much weaker than that on pure AChE. However, in the presence of a low dose of diisopropyl fluorophosphate, just enough to inhibit BuChE but not AChE, the IC50s of itopride against ChE activities were found to be about 0.5 1tM. In conclusion, itopride exerts reversible and a "mixed" type of inhibition preferably against AChE. The IC50 of itopride for electric eel and guinea pig gastrointestinal AChE inhibition was 200 times and 50 times as large as that of neostigmine, respectively.

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“…In contrast, domperidone, a gastroprokinetic agent which is reported to enhance the ACh release from the stomach via the blockade of dopamine D2 receptor (12), did not affect the peristalsis. The stimulation of ACh release may not result in the enhanced peristalsis in the ileum.…”

mentioning

confidence: 69%